Reaction Details |
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Target | Histamine H3 receptor |
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Ligand | BDBM50414387 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_576568 (CHEMBL1034549) |
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Ki | 2.51±n/a nM |
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Citation | Lim, HD; Istyastono, EP; van de Stolpe, A; Romeo, G; Gobbi, S; Schepers, M; Lahaye, R; Menge, WM; Zuiderveld, OP; Jongejan, A; Smits, RA; Bakker, RA; Haaksma, EE; Leurs, R; de Esch, IJ Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies. Bioorg Med Chem17:3987-94 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histamine H3 receptor |
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Name: | Histamine H3 receptor |
Synonyms: | G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4) |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 48691.47 |
Organism: | Homo sapiens (Human) |
Description: | Binding assays were using CHO cells stably expressing hH3R receptors. |
Residue: | 445 |
Sequence: | MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
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BDBM50414387 |
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n/a |
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Name | BDBM50414387 |
Synonyms: | CHEMBL1743881 |
Type | Small organic molecule |
Emp. Form. | C14H17BrN4S |
Mol. Mass. | 353.281 |
SMILES | NC(SCCCc1cnc[nH]1)=NCc1ccc(Br)cc1 |w:11.12| |
Structure |
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